Kim Jung Suk, Choi Yoo Jin, Woo Mi Ran, Cheon Seunghyun, Ji Sang Hun, Im Daseul, Ud Din Fakhar, Kim Jong Oh, Youn Yu Seok, Oh Kyung Taek, Lim Soo-Jeong, Jin Sung Giu, Choi Han-Gon
College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea.
Department of Pharmacy, Quaid-I-Azam University, Islamabad 45320, Pakistan.
Carbohydr Polym. 2021 Nov 1;271:118433. doi: 10.1016/j.carbpol.2021.118433. Epub 2021 Jul 14.
The purpose of this study was to use hydroxypropyl-β-cyclodextrin (HP-β-CD) as a novel carrier in solid SNEDDS and solid dispersions to enhance the solubility and oral bioavailability of poorly water-soluble dexibuprofen. The novel dexibuprofen-loaded solid SNEDDS was composed of dexibuprofen, corn oil, polysorbate 80, Cremophor® EL, and HP-β-CD at a weight ratio of 45/35/50/15/100. This solid SNEDDS spontaneously formed a nano-emulsion with a size of approximately 120 nm. Unlike the conventional solid SNEDDS prepared with colloidal silica as a carrier, this dexibuprofen-loaded solid SNEDDS exhibited a spherical structure. Similar to the dexibuprofen-loaded solid dispersion prepared with HP-β-CD, the transformation of the crystalline drug to an amorphous state with no molecular interactions were observed in the solid SNEDDS. Compared to the solid dispersion and dexibuprofen powder, solid SNEDDS significantly enhanced drug solubility and AUC. Therefore, HP-β-CD is a novel potential carrier in SNEDDS for improving the oral bioavailability of dexibuprofen.
本研究的目的是使用羟丙基-β-环糊精(HP-β-CD)作为固体自乳化药物传递系统(SNEDDS)和固体分散体中的新型载体,以提高难溶性右旋布洛芬的溶解度和口服生物利用度。新型载药固体SNEDDS由右旋布洛芬、玉米油、聚山梨酯80、聚氧乙烯蓖麻油EL和HP-β-CD按45/35/50/15/100的重量比组成。这种固体SNEDDS自发形成了粒径约为120nm的纳米乳液。与以胶体二氧化硅为载体制备的传统固体SNEDDS不同,这种载药固体SNEDDS呈现出球形结构。与用HP-β-CD制备的载药固体分散体相似,在固体SNEDDS中观察到结晶药物转变为无定形状态且无分子相互作用。与固体分散体和右旋布洛芬粉末相比,固体SNEDDS显著提高了药物溶解度和药时曲线下面积(AUC)。因此,HP-β-CD是SNEDDS中一种新型的潜在载体,可用于提高右旋布洛芬的口服生物利用度。